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442640 L3MBTL1 Ligand, UNC669 - Calbiochem

442640
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₅H₂₀BrN₃O

Pricing & Availability

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442640-25MG
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      Glass bottle 25 mg
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      Description
      OverviewA nicotinamido-pyrrolidine compound that targets the second MBT (Malignant Brain Tumor) module of "chromatin lock" L3MBTL1 (Lethal 3 MBT-Like protein 1; Kd = 5 µM by Isothermal titration calorimetry) that "reads"/binds mono- and dimethyl-lysine modified histones as well as other proteins involved in transcription, such as p53 and Rb, via methylation-dependent recognition. Shown to effectively compete against FAM-labeled, monomethylated Histone H3 (1-15) peptide (H3K9Me1) binding to L3MBTL1 (Kd = 10 µM in a FP displacement assay) and exhibit higher affinity toward L3MBTL1 than L3MBTL3 and L3MBTL4 (IC50 = 6, 35, and 69 µM, respectively, in a luminescent peptide competitive binding assay), while displaying no detectable binding toward four other methyl-lysine-binding proteins, the BMT domain-containing SFMBT1 and MBTD1, the PHD (Plant Homeodomain) finger-containing PHF13 (PHD finger 13), and the chromo domain-containing CBX7 (chromobox 7). As of end of 2012, no published data is available regarding the molecule's permeability or biological activity in cells.
      Catalogue Number442640
      Brand Family Calbiochem®
      Synonyms5-Bromo-N-(4-(pyrrolidinyl)piperidinyl)nicotinamide
      References
      ReferencesHerold, J.M., et al. 2011. J. Med. Chem. 54, 2504.
      Product Information
      FormPale orange-yellow solid
      Hill FormulaC₁₅H₂₀BrN₃O
      Chemical formulaC₁₅H₂₀BrN₃O
      Hygroscopic Hygroscopic
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥95% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      L3MBTL1 Ligand, UNC669 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      L3MBTL1 Ligand, UNC669 - Calbiochem Certificates of Analysis

      TitleLot Number
      442640

      References

      Reference overview
      Herold, J.M., et al. 2011. J. Med. Chem. 54, 2504.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision02-April-2012 JSW
      Synonyms5-Bromo-N-(4-(pyrrolidinyl)piperidinyl)nicotinamide
      DescriptionA nicotinamido-pyrrolidine compound that targets the second MBT (Malignant Brain Tumor) module of "chromatin lock" L3MBTL1 (Lethal 3 MBT-Like protein 1; Kd = 5 µM by Isothermal titration calorimetry) that "reads"/binds mono- and dimethyl-lysine modified histones as well as other proteins involved in transcription, such as p53 and Rb, via methylation-dependent recognition. Shown to effectively compete against FAM-labeled, monomethylated Histone H3 (1-15) peptide (H3K9Me1) binding to L3MBTL1 (Kd = 10 µM in a FP displacement assay) and exhibit higher affinity toward L3MBTL1 than L3MBTL3 and L3MBTL4 (IC50 = 6, 35, and 69 µM, respectively, in a luminescent peptide competitive binding assay), while displaying no detectable binding toward four other methyl-lysine-binding proteins, the BMT domain-containing SFMBT1 and MBTD1, the PHD (Plant Homeodomain) finger-containing PHF13 (PHD finger 13), and the chromo domain-containing CBX7 (chromobox 7). As of end of 2012, no published data is available regarding the molecule's permeability or biological activity in cells.
      FormPale orange-yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₅H₂₀BrN₃O
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (50 mg/ml) or H₂O (2.5 mg/ml)
      Storage -20°C
      Hygroscopic
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesHerold, J.M., et al. 2011. J. Med. Chem. 54, 2504.